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Inhibition of HIV-1 capsid assembly: optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold.

Abstract：

:A uHTS campaign led to the discovery of a 5-(5-furan-2-ylpyrazol-1-yl)-1H-benzimidazole series that inhibits assembly of HIV-1 capsid. Synthetic manipulations at N1, C2 and C16 positions improved the antiviral potency by a . The X-ray structure of 33 complexed with the capsid N-terminal domain allowed identification of major interactions between the inhibitor and the protein.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tremblay M,Bonneau P,Bousquet Y,DeRoy P,Duan J,Duplessis M,Gagnon A,Garneau M,Goudreau N,Guse I,Hucke O,Kawai SH,Lemke CT,Mason SW,Simoneau B,Surprenant S,Titolo S,Yoakim C

doi

10.1016/j.bmcl.2012.10.034

subject

Has Abstract

pub_date

2012-12-15 00:00:00

pages

7512-7

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01312-1

journal_volume

22

pub_type

杂志文章

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